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英文药名: Oxsoralen (methoxsalen capsules)
中文药名: 甲氧沙林胶囊
生产厂家: ICN Pharmaceuticals
药品名称
通用名称：甲氧沙林
英文名：Methoxsalen
其它中文名：8-甲氧补骨脂素、8-甲氧基补骨脂素、甲氧补骨脂素、敏白灵
其它英文名：8-Methoxypsoralen、Meladinin、Methoxypsoralen、Methoxysoralen
规格
甲氧沙林硬胶囊10mg,甲氧沙林乳液 30ml.
药理作用
药效学
本品为补骨脂素的衍生物，有光感活力。使引起表皮红斑、黑色素和细胞毒的确切机制尚不清楚，但能使黑色素形成细胞中的酪氨酸酶活力增加，亦可抑制 DNA合成、细胞分裂和表皮更替，有效的色素形成需要有机能的黑色素细胞存在。
药动学
口服约 95％从胃肠道吸收，有些患者效果差，推测与吸收不良有关。蛋白结合率高。可被320～400nm的长波紫外线A激活，最大作用波长为 365nm。Ｔ1/2硬胶囊为 1.1小时，软胶囊为 2小时。白癜风患者需 6个月或更长时间起效，银屑病需30余次(10周或更长时间)，皮肤对日光敏感性增加为l小时，皮肤晒黑数天内。光敏达峰时间硬胶囊为 3.9～4.25小时，软胶囊为1.5～2.1小时。平均最小红斑量(MED)软胶囊的要比硬胶囊每 1平方厘米的能量少。与 250ml牛奶进服时血药浓度峰值硬胶囊为l.5～6小时(平均 3小时)，软胶囊为 0.5～4小时(平均 1.8小时)。作用时间，增加皮肤对日光敏感约 8小时。本品在肝脏代谢，代谢物主要从肾脏排泄，8小时内排出 80～90％，24小时内95％，粪便排出 4～10％。
适应症
本品需与长波紫外线 A(UVA)合用(两者合用方式称PUVA)治疗白癜风、银屑病、蕈样肉芽肿；PUVA亦用于治疗斑秃、异位性皮炎、湿疹、扁平苔藓，增加皮肤的日光耐受性。
用法用量
(1)治牛皮癣：
①加黑光照射法：方法同补骨脂素，1次服用量为 30—50mg。
②加紫外线照射法：饭后服20—50mg， 1小时后矿泉水全身浸浴 20—30分钟， 2小时后长波紫外线照射，照射量从最小红斑量开始逐渐增加。外用者于照射前，距正常皮肤 0.5cm处的皮损范围内涂本品的 0.5％配剂。按此法每日治疗 1次(星期日休息)，持续至皮损消失后逐渐减少治疗次数，直至每周或每月 1次，长期巩固治疗。据报道，按本法治疗 46例，治愈(皮损全部消失) 45例，显效 1例。平均治疗 9次见效， 60次痊愈。
(2)治白癜风： 0.1溶液(白癜风溶液)涂搽。
1．硬胶囊剂成人常用量：
①白癜风，在照射 UVA前 2— 4小时口服20mg，每周 2— 3次(至少相隔 48小时)，日光照射时，对淡肤色者首次不超过 15分钟，对中等度肤色者，不超过20分钟，对深肤色者不超过25分钟，根据出现红斑和压痛情况，以后每次治疗可增加5分钟，如采用人工光源照射时，首次照射时间不超过日光照射发生红斑时间的一半；
②银屑病或草样肉芽肿，在照射 UVA前24小时，按体重口服0.6mg/kg，每周 2— 3次(至少相隔 48小时)，暴光时间需按照采用特殊光源的说明根据皮肤类型和治疗效应而定，暴光次数可逐渐减少至维持治疗。
下面为参照体重的通常剂量表。
体重（kg） 剂量（mg）
<30 10
30－50 20
51－65 30
66－80 40
81－90 50
91－115 60
>115 70
12岁以上儿童剂量同成人常用量，12岁以下禁用。
2．软胶囊成人常用量：治疗银屑病，在照射 UVA前 1.5— 2小时按体重口服0.4mg/kg，每周 2— 3次，余同硬胶囊。
3．外用洗剂涂在白癜风损害上，等 1一 2分钟待干，再涂 1次，2— 2.5小时照光；随后以肥皂和水洗净，盖上遮光物。日光照射开始不超过 1分钟，以后逐渐增加。人工光源首次照射时间不超过暴晒日光产生红斑的一半时间，通常3— 5天或7天照射1次。
任何疑问,请遵医嘱!
禁用/慎用
下列情况应禁用：严重心血管病、白化病、夏令水疱病、传染源白斑、急性红斑狼疮、皮肌炎、多形性日光疹、卟啉病、着色性干皮病、白内障、肝功能损害。
下列情况应慎用：慢性感染、胃肠道疾病、皮肤癌病史、日光敏感家族史，新近接受过 X射线或细胞毒治疗、砷剂、煤焦油和 UVB治疗者。
给药说明
对长期应用本品的患者，需定期随访抗核抗体试验、血象、肝肾功能、需注意有无白内障、黑色素瘤或皮肤癌的发生。
①口服可能需在 6— 8周起作用，不要随意增加药物剂量或 UVB照射。硬胶囊剂与食物或牛奶一起服(软胶囊剂与低脂肪饮食或低脂肪牛奶一起服)，以减少胃肠道刺激；
②治疗中不要将本品软胶囊与硬胶囊互换，因前者比后者具较大生物有效性和较早发生光敏；
③有些临床医师认为治疗银屑病经15次照射无效应时，需增加剂量，通常本品剂量不需增加；
④本品剂量根据体重计算，倘患者体重改变，不要改变剂量，如体重改变显著，可调整 UVA暴光时间；
⑤倘用作增加皮肤对日光的耐受性，治疗限制在 14天内；
⑥暴晒日光或紫外线时间需根据患者皮肤类型和耐受性而个体化，在高原和中午日光暴晒时间需缩短；
⑦对有红皮病型银屑病患者采取同日光过敏皮肤类型相同的治疗；
⑧采用PUVA治疗前24小时和治疗后 8小时，需保护皮肤勿晒阳光(包括透过玻璃窗或多云天气)，穿长袖衬衫、宽松长裤、阔边帽、戴手套和具有保护系数至少15遮光物质涂在不能以衣服遮盖的部位，口唇涂防光系数至少 15的唇膏；
⑨在面、腹、臀等部位，最快出现色素再生，四肢和手足较迟；
⑩倘皮肤出现烧灼或水泡，暂停治疗；倘发生肝功能受损，需减少本品剂量或停止治疗；对超剂量的治疗：在 2— 3小时内，导引呕吐，将患者移至暗室至少24小时，如发生意外的照射过度或曝晒日光，可将患者移至暗室至少24小时，如在 24小时内出现Ⅱ度烧伤(显著红斑而无水肿)，提示开始潜在的严重烧伤信号，因对 PUVA的红斑反应峰通常约发生在口服本品 48小时后，根据发生的范围和严重度进行烧伤的对症治疗。
外用比口服更能引起不易预料的光敏感效应，仅适于在小于 10平方立米的面积上涂用，照射日光或 UVA后将所涂药品去掉；照射日光或 UVA的时间亦需根据患者的皮肤类型和耐受性适当调节。外用时造成表皮中的本品浓度较口服时为高，故通常采用的 UVA剂量较口服时为低。在外用和 UVA照射治疗后，至少 12— 48小时避免日光照射。当色素比红斑形成早且很长时间时，皮肤可以对本品产生耐受性，色素沉着过度可减少以后的效应。稀释至 1：1000或 1：10000的浓度可避免严重反应。色素形成通常在治疗数周后开始，但显著色素再生需经6— 9个月，需周期性再治疗，以保持所有新生色素。
不良反应
①曾报道可发生白内障；
②动物实验发现本品能诱发 UVA的致癌作用，对人有增加鳞状细胞癌发生的危险性，特别是患者存在危险因子时如淡色皮肤，对日光敏感，皮肤癌病史，暴露于电离放射，过多在日光中曝晒，或以焦油和紫外线B(UVB)、砷或外用氮芥治疗过的患者；
③皮肤早老表现；
④中毒性肝炎；
⑤紫外线超剂量或超时间照射的症候为皮肤起水泡和脱屑、发红和疼痛、特别是足和小腿的肿胀；
⑥还可有皮肤瘙痒、恶心、头晕、头痛、精神抑郁、神经质和失眠。对骨髓造血系统有影响,可有白细胞减少.
药物相互作用
治疗期间不食用含有呋喃香豆素的食物(如酸橙、无花果、香菜、芥末、胡萝卜或芹菜)，以免发生附加的光毒性危险；与其他光敏性药物亦不得同时服用；与吩噻嗪类药物同用可加剧对脉络膜、视网膜和晶体的眼内光化学损伤。
Oxsoralen kapszula
Oxsoralen Lotion is used for:
Treating vitiligo in combination with controlled doses of ultraviolet A (UVA) or sunlight. It may also be used for other conditions as determined by your doctor.
Oxsoralen Lotion is a psoralen used in combination with light therapy. It works by making the skin more sensitive to UV light. It appears that this sensitivity results in damage to the skin cells when UV light treatment is given. Damaged skin cells grow more slowly and the rate of tissue growth is reduced.
Do NOT use Oxsoralen Lotion if:
• you are allergic to any ingredient in Oxsoralen Lotion or to similar medicines
• you have a light-sensitive disease (eg, the blood disease porphyria, lupus, xeroderma pigmentosum)
• you have a history of melanoma or certain types of skin cancer
• your skin is sensitive to the sun or light
Contact your doctor or health care provider right away if any of these apply to you
Before using Oxsoralen Lotion:
Some medical conditions may interact with Oxsoralen Lotion. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:
• if you are pregnant, planning to become pregnant, or are breast-feeding
• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement
• if you have allergies to medicines, foods, or other substances
• if you are fair-skinned, have a history of coal tar UV treatment, or ionizing radiation, or have taken arsenic compounds or oral psoralen UVA treatment
• if you have other skin conditions, an infection, or a history of heart or blood vessel disease
Some MEDICINES MAY INTERACT with Oxsoralen Lotion. Tell your health care provider if you are taking any other medicines, especially any of the following:
• Hydantoins (eg, phenytoin) because the effectiveness of Oxsoralen Lotion may be decreased
This may not be a complete list of all interactions that may occur. Ask your health care provider if Oxsoralen Lotion may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.
How to use Oxsoralen Lotion:
Use Oxsoralen Lotion as directed by your doctor. Check the label on the medicine for exact dosing instructions.
• Oxsoralen Lotion is usually applied at your doctor's office or a clinic.
• Oxsoralen Lotion is applied only in small well-defined lesions and preferably on lesions that can be protected by clothing or sunscreen from later exposure to UVA.
• If you miss a dose of Oxsoralen Lotion, contact your doctor right away.
Ask your health care provider any questions you may have about how to use Oxsoralen Lotion.
Important safety information:
• After you begin Oxsoralen Lotion and light therapy, several weeks to months may pass before you see an improvement in your condition.
• Do not sunbathe for at least 24 hours before receiving Oxsoralen Lotion and light therapy. After your treatment, avoid any exposure to sunlight for at least 8 hours. This includes indirect light through a window or on cloudy days. If you can not avoid exposure to sunlight, wear protective clothing, or use a sunscreen with a sun protective factor (SPF) of 15 or greater, as directed by your doctor. Protect all areas of the body, including lips, from sun exposure. Do not sunbathe or use a tanning booth without checking with your doctor and wait at least 48 hours after your treatment.
• Serious burns from either UV light or sunlight (even through a window glass) can occur if the recommended doses of Oxsoralen Lotion or exposure schedules are not maintained.
• The treated area may be highly sensitive to sunlight for several days and may cause severe burning if exposed to additional UV or sunlight. Protect the treated areas with clothing or sunscreen.
• Return of skin color may begin after a few weeks, but significant color may require 6 to 9 months of treatment.
• Exposure to sunlight or UV radiation may cause early aging of the skin.
• During treatment with Oxsoralen Lotion and UVA light, wear total UVA absorbing/blocking goggles designed to provide maximal protection of the eyes.
• Protect stomach skin, breasts, genitals, and other sensitive areas for about one third of the exposure time until tanning occurs.Unless affected by disease, male genitals should be shielded.
• Be careful using Oxsoralen Lotion with other light-sensitizing medicines. Tell your doctor if you are taking any of the following medicines: anthralin, coal tar and derivatives, griseofulvin, phenothiazines, nalidixic acid, fluoroquinolone antibiotics, halogenated salicylanilides, bacteriostatic soaps, staining dyes (eg, methylene blue, toluidine blue, rose bengal, methyl orange), sulfonamides, tetracyclines, or thiazide diuretics.
• LAB TESTS may be performed to monitor your progress or to check for side effects. Be sure to keep all doctor and lab appointments.
• Use Oxsoralen Lotion with caution in the ELDERLY because they may be more sensitive to its effects.
• Oxsoralen Lotion is not recommended for use in CHILDREN younger than 12 years of age. Safety and effectiveness in this age group have not been confirmed.
• PREGNANCY and BREAST-FEEDING: If you become pregnant, discuss with your doctor the benefits and risks of using Oxsoralen Lotion during pregnancy. It is unknown if Oxsoralen Lotion is excreted in breast milk. If you are or will be breast-feeding while you are using Oxsoralen Lotion, check with your doctor or pharmacist to discuss the risks to your baby.
Possible side effects of Oxsoralen Lotion:
All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:
Dryness or redness of the skin; itching.
Seek medical attention right away if any of these SEVERE side effects occur:
Severe allergic reactions (rash; hives; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); blistering; burns on the treated area from overexposure to UVA or sunlight; severe swelling or redness of the skin; swelling of the feet or lower legs; tenderness.
This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.
If OVERDOSE is suspected:
Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center (http://www.aapcc.org), or emergency room immediately. Symptoms may include blisters; burns. Oxsoralen Lotion may be harmful if swallowed.
Proper storage of Oxsoralen Lotion:
Oxsoralen Lotion is usually handled and stored by a health care provider. If you are using Oxsoralen Lotion at home, store Oxsoralen Lotion as directed by your pharmacist or health care provider. Keep Oxsoralen Lotion out of the reach of children and away from pets.
General information:
• If you have any questions about Oxsoralen Lotion, please talk with your doctor, pharmacist, or other health care provider.
• Oxsoralen Lotion is to be used only by the patient for whom it is prescribed. Do not share it with other people.
• If your symptoms do not improve or if they become worse, check with your doctor.
This information is a summary only. It does not contain all information about Oxsoralen Lotion. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider. |
